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Divalent tranylcypromine derivative as lysine-specific demethylase 1 inhibitor

文献类型：期刊论文

作者Sun, Yin1,2; Li, Na1,3; Su, Mingbo3,4; Wang, Xiaowen1; Zhao, Dongmei2; Xiong, Bing1,3; Zhou, Yubo3,4; Liu, Tongchao1; Chen, Yue-Lei1,3
刊名MEDICINAL CHEMISTRY RESEARCH
出版日期2021-01-20
页码8
关键词Divalent tranylcypromine LSD1 inhibitor MV4-11 antiproliferative activity CD86 mRNA expression Linker Selectivity
ISSN号1054-2523
DOI10.1007/s00044-020-02689-z
通讯作者Zhao, Dongmei(dongmeiz-67@163.com) ; Zhou, Yubo(ybzhou@simm.ac.cn) ; Liu, Tongchao(tongchao_liu@simm.ac.cn)
英文摘要Tranylcypromine (TCP) is a useful pharmacophore for lysine-specific demethylase 1 (LSD1) inhibitors. Based on the mode of action (MOA) of TCP and structure of LSD1, divalent TCP derivatives with aliphatic and benzylic linkers were designed, synthesized, and evaluated for their LSD1 inhibitory activity, MV4-11 antiproliferative activity, and CD86 mRNA expression enhancement. All ten new compounds showed improved activity against LSD1 than TCP and GSK2879552. Several compounds with rigid aliphatic linkers demonstrated nanomolar enzymatic and cellular activities, as well as good MAO-A/B selectivity. Further supported by their significant CD86 mRNA expression enhancement effect, divalent TCP derivative can be promising lead for new LSD1 inhibitors.
资助项目National Natural Science Foundation of China[21877121] ; National Natural Science Foundation of China[81673309] ; National Natural Science Foundation of China[81703544] ; China Postdoctoral Science Foundation[2019M661671] ; program for Innovative Research Team of the Ministry of Education ; program for Liaoning Innovative Research Team at Shenyang Pharmaceutical University
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000608930200001
出版者SPRINGER BIRKHAUSER
源URL[http://119.78.100.183/handle/2S10ELR8/296000]  
专题中国科学院上海药物研究所
通讯作者Zhao, Dongmei; Zhou, Yubo; Liu, Tongchao
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
2.Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Lu, Shenyang 110016, Peoples R China
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
4.Natl Ctr Drug Screening, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Sun, Yin,Li, Na,Su, Mingbo,et al. Divalent tranylcypromine derivative as lysine-specific demethylase 1 inhibitor[J]. MEDICINAL CHEMISTRY RESEARCH,2021:8.
APA Sun, Yin.,Li, Na.,Su, Mingbo.,Wang, Xiaowen.,Zhao, Dongmei.,...&Chen, Yue-Lei.(2021).Divalent tranylcypromine derivative as lysine-specific demethylase 1 inhibitor.MEDICINAL CHEMISTRY RESEARCH,8.
MLA Sun, Yin,et al."Divalent tranylcypromine derivative as lysine-specific demethylase 1 inhibitor".MEDICINAL CHEMISTRY RESEARCH (2021):8.

入库方式： OAI收割

来源：上海药物研究所

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